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At least 145 records · Page 8Linked to original sources
PubMed1984

Correlation between in vitro and in vivo response to androgens in patients with aplastic anemia.

In an attempt to predict the clinical response to androgens, the effects of added fluoxymesterone (FMT) on the in vitro growth of marrow erythroid progenitors (CFU-E) were examined in 15 patients with aplastic anemia and 6 control subjects with normal marrow morphology. In the control group, the addition of FMT enhanced the growth of CFU-E in vitro, the maximum absolute increase being dependent on the basal number of CFU-E. In 10 out of the 11 aplastic anemia patients who responded to androgens in vivo. FMT enhanced the growth of CFU-E in vitro. In this group, there was a positive correlation between the basal number of CFU-E and the maximum absolute increase of CFU-E induced by FMT. In patients who did not respond to androgens in vivo, all except one showed no increase in the growth of CFU-E in vitro by the addition of FMT. Furthermore, in four out of seven patients examined prior to androgen therapy, the addition of FMT enhanced the in vitro growth of CFU-E. Androgen therapy in vivo resulted in marked hematological improvements in all of these four patients. Two out of the remaining three patients in whom FMT did not enhance the in vitro growh of CFU-E failed to respond in androgen therapy. These results indicate that an in vitro CFU-E culture system to the presence of FMT may be helpful in predicting the response to androgens in vivo in patients with aplastic anemia.

Adolescent↗
PubMed1986

Effects of a potent LHRH-agonist on the pituitary gonadal axis with and without testosterone substitution.

In this study we investigated the effect of low and high dosages of a potent LHRH agonist on the pituitary-gonadal axis with special consideration to the effect on the tubular compartment of the testis. Included were 3 treatment groups: the probands in Group I were treated with 3 X 50 micrograms HOE 766/week intranasally for 5 months; in Group II with 3 X 100 micrograms HOE 766 intranasally/day for 6 months and in Group III with 3 X 200 micrograms HOE 766 intranasally plus 5 mg fluoxymesterone orally/day for 5 months. With the low dose (Group I) no changes in the seminal parameters measured could be observed whereas LH and FSH levels increased in plasma, testosterone showed no change compared to pretreatment values. When high dosages/day of a potent LHRH agonist were administered without androgen replacement (Group II) pronounced decrease of LH and FSH took place, the testosterone plasma levels approached the female range. Spermatogenesis was arrested. The agonist plus androgen replacement (Group III) counteracted the suppression of spermatogenesis.

Administration, Intranasal↗
PubMed1985

Short term high density systemic therapy for metastatic breast cancer.

Twenty-three patients with metastatic breast carcinoma were induced with a complex systemic therapy regimen in an attempt to ascertain if a complete remission rate greater than 50% could be obtained with intensive drug exposure. The durability of the remissions was observed by discontinuing therapy after 3 cycles in complete remission or after 6 cycles of treatment, whichever was longer. In 13 patients consolidation radiation therapy to the pre-treatment sites of disease was administered after discontinuing systemic therapy. Each 28 day cycle of the drug regimen consisted of pulses of adriamycin, vincristine, dibromodulcitol, prednisone, methotrexate with leukovorin rescue, hexamethylmelamine, bleomycin (discontinued after entry #17), fluoxymesterone, and tamoxifen. Eighteen of the 23 patients achieved complete remissions (78%) and 3 had partial remissions. The median times to treatment failure and survival were, respectively, 12.3 and 19.4 mos. The times for complete remission patients were, respectively, 13.5 and 23.9 mos. Consolidation radiotherapy at greater than or equal to 40 Gy to drug induced pre-study sites of complete remission was associated with first relapses at pre-study sites in 5/30 (17%) instances, compared to 21/35 (60%) in sites not receiving radiotherapy. Side-effects were commensurate with the intensity of the treatment program and are detailed in the text. Although the achievement of a high complete remission rate is promising, the failure to extend their duration beyond that of historical data suggests that additional conceptual and therapeutic approaches need to be explored.

Altretamine↗
PubMed1981

Steroid-induced concentric membrane whorls in dog liver.

When daily doses of 10 mg/kg of the androgenic steroids fluoxymesterone, methyltestosterone, testosterone propionate, oxymetholone and mepitiostane were administered to adult male and female beagle dogs for 6 months, concentric membrane whorls were produced in the hepatocytes of all groups. The whorls frequently had a central core mainly composed of lipids or mitochondria and the membranes of the whorls, consisting of paired membranes, continued to the smooth or granular endoplasmic reticulum at the periphery of the structures.

Anabolic Agents↗
PubMed1976

Impotence therapy and cancer of the prostate.

Prostate cancer developed in two male patients being treated with fluoxymesterone for erectile impotence. It is suggested that the current increased interest in and therapy for sexual dysfunction be accompanied by an awareness of a possible causal relationship between exogenous androgens and prostrate cancer.

Adenocarcinoma↗
PubMed1991

Treatment with anabolic steroids increases the activity of the mitochondrial outer carnitine palmitoyltransferase in rat liver and fast-twitch muscle.

Treatment of male rats with the anabolic steroids fluoxymesterone or methylandrostanolone increased the activity of the outer carnitine palmitoyltransferase in liver and fast-twitch muscle mitochondria. This effect was not potentiated by physical exercise and was not observed in heart and slow-twitch muscle mitochondria. Anabolic steroids did not affect the sensitivity of the liver enzyme to inhibition by malonyl-CoA. The data presented herein suggest that androgens may have an important physiological role in the regulation of fatty acid oxidation in liver and fast-twitch muscle mitochondria. In addition, our results are at odds with the notion that (most of) the metabolic effects of anabolic steroids on muscle are only evident when physical training is parallely performed.

Anabolic Agents↗
PubMed1987

Androgen depletion and repletion as a means of potentiating the effect of cytotoxic chemotherapy in advanced prostate cancer.

Seventy-five patients with stage D-2 prostate cancer refractory to orchiectomy have been entered in a controlled trial to test whether androgen priming enhances the efficacy of chemotherapy. All patients are treated with aminoglutethimide and hydrocortisone as a means of achieving medical adrenalectomy and are given cyclic i.v. chemotherapy with cytoxan, adriamycin and 5-fluorouracil. Patients in the stimulation arm (N = 39) receive, in addition, fluoxymesterone (5 mg p.o. b.i.d.) for 3 days before and on the day of chemotherapy. A similar response rate was observed in the stimulation and control arm (83% vs 74% respectively) when the analysis was restricted to evaluable patients. When all patients were included, a significantly higher response rate was observed in the control arm (64% vs 49%, P less than 0.05) as a result of the larger fraction of unevaluable patients in the stimulation arm (41% vs 14%). Median duration of response is 9 months in the stimulation and 10 months in the control arm. Median overall survival in the stimulation and control group is 12 months and 16 months respectively. Significant toxicity consisting of exacerbation of bone pain and, in two patients, development of reversible spinal cord compression was observed following androgen priming. Our results suggest that combined medical adrenalectomy and chemotherapy are highly effective in the treatment of advanced prostate cancer. Thus far, no additional benefit has been observed with androgen priming.

Aminoglutethimide↗
PubMed1994

Aberrant androgen action and increased size of tandem CAG repeat in androgen receptor gene in X-linked recessive bulbospinal neuronopathy.

Plasma levels of testosterone, luteinizing hormone (LH) and follicle-stimulating hormone (FSH) after 3 or 6 days of administration of the synthetic androgenic hormone fluoxymesterone (10 mg/day) were measured in 26 patients with X-linked recessive bulbospinal neuronopathy (X-BSNP) and 22 age-matched male controls. The testosterone, LH and FSH levels in the controls were markedly suppressed after administration, but in the patients with X-BSNP, they were suppressed significantly less. The level of suppression varied considerably with the patients, and those of plasma testosterone and FSH were significantly correlated with the number of CAG repeats in the androgen receptor gene. These findings suggest that the androgen action was aberrantly transduced in the target organs in the patients with X-BSNP and which is related to the elongated CAG repeat in the androgen receptor gene.

Adult↗
PubMed1984

Direct action of androgen on hot flushes in the human male.

Hot flushes (HF) were demonstrated definitively in a hypogonadal man by continuous recordings of finger temperature, skin resistance and subjective symptoms. The magnitudes and temporal interrelationships of these physiological changes were similar to those previously observed in oophorectomized women. HF were abolished by injections of methyl testosterone (MT) and during oral administration of fluoxymesterone (FM), a non-aromatizable androgen. Increases of the non-SHBG bound fractions of T and E2 were noted during MT therapy, either of which may have been responsible for suppression of HF. No significant changes of the non-SHBG bound levels of E2 were observed during FM ingestion. These data confirm that typical HF occur in the male and support the concept that androgen acts directly on the central nervous system without requiring aromatization to estrogen in the brain or other tissues.

Adult↗
PubMed1995

Toxic effects of anabolic-androgenic steroids in primary rat hepatic cell cultures.

Hepatic complications in athletes and bodybuilders after abusing anabolic-androgenic steroids (AAS) have been reported. Hepatic injury, including cholestasis, peliosis hepatis, hyperplasia, and tumors, have been attributed to abuse of the 17 alpha-alkylated AAS. Some of these pathological conditions have been reversed when individuals were converted to nonalkylated AAS regimens. The purpose of this study was to determine and compare the direct toxic effects of commonly abused AAS (both 17 alpha-alkylated and nonalkylated) in primary hepatic cell cultures. Primary cultures, established from 60-day-old Sprague-Dawley rats, were exposed to doses of 1 x 10(-8), 1 x 10(-6), and 1 x 10(-4)M 19-nortestosterone, fluoxymesterone, testosterone cypionate, stanozolol, danazol, oxymetholone, testosterone, estradiol, and methyltestosterone for 1, 4, and 24 hr. Lactate dehydrogenase (LDH) release, neutral red (NR) retention, and glutathione (GSH) depletion were evaluated to determine plasma membrane damage, cell viability, and possible oxidative injury, respectively. Those cultures exposed to the 17 alpha-alkylated AAS, methyltestosterone and stanozolol, at doses of 1 x 10(-4) M for 24 hr and the 17 alpha-alkylated AAS, oxymetholone, at 1 x 10(-4) M for 4 and 24 hr showed significant increased in LDH release and decreases in NR retention while there were no significant differences with the nonalkylated steroids (testosterone cypionate, 19-nortestosterone, testosterone, and estradiol). GSH depletion was evaluated in cultures treated with 1 x 10(-8), 1 x 10(-6), and 1 x 10(-4) M concentrations of methyltestosterone, stanozolol, and oxymetholone for 1, 2, 4, and 6 hr. Cultures exposed to 1 x 10(-4) M oxymetholone were significantly depleted of GSH at 2, 4, and 6 hr; cultures exposed to 1 x 10(-4) M methyltestosterone were significantly depleted of GSH at 4 and 6 hr; and cultures exposed to stanozolol were not significantly depleted of GSH at any of the time periods tested. These data indicate that the 17 alpha-alkylated steroids (methyltestosterone, oxymetholone, and stanozolol) are directly toxic to hepatocytes, whereas the nonalkylated steroids (testosterone cypionate, 19-nortestosterone, testosterone, and estradiol) show no effects at similar doses. These data demonstrate a trend toward a structural-activity relationship to AAS-induced toxicity in primary cultures of rat hepatocytes.

Anabolic Agents↗
PubMed1979

The effect of synthetic androgens on the hypothalamic-pituitary-gonadal axis in boys with constitutionally delayed growth.

Serial concentrations of basal serum LH, FSH, testosterone, and LH and FSH responses to intravenous gonadotropin-releasing hormone were measured before and during six months of administration of fluoxymesterone or oxandrolone in 14 boys with constitutionally delayed growth and adolescence, in order to assess the effects of these androgens on maturation of the hypothalamic-pituitary-gonadal axis. Before therapy all boys had normal hormonal responses based on bone age. At the end of six months therapy 10 of the 14 boys had lower LH responses (34 to 89% reduction) to GnRH without consistent changes in FSH responses. With both androgens, there there was significant suppression of both basal serum FSH and testosterone. Eleven boys were restudied six months after completion of therapy; basal serum LH, FSH, and testosterone and responses to GnRH were equal to or greater than pretreatment levels, indicating recovery or progressive maturation of the HPGA. All boys had increased growth velocity and imporved weight gain without excessive bone age advancement; all had improved psychosocial adjustment.

Adolescent↗
PubMed1979

Oxandrolone therapy in patients with Turner syndrome.

Long-term, low-dosage androgen treatment of patients with Turner syndrome results in more rapid growth and significantly greater adult height than in control patients who receive only estrogen for pubertal development. Seventeen patients treated with oxandrolone for one year and ten treated for two years had significantly greater growth velocities during than before treatment. Mean adult height of 25 patients treated with oxandrolone, fluoxymesterone, or both was significantly taller than the height of adult patients with Turner syndrome treated with estrogen only. Excessive skeletal maturation was not generally observed.

Body Height↗
PubMed1977

Androgen therapy of a varicocele.

A case of asthenospermia and decreased semen volume with consequent infertility is reported. The patient had large bilateral varicoceles but refused an operation. Significant improvement of volume and motility occurred after treatment with fluoxymesterone and pregnancy was achieved.

Adult↗
PubMed2003

Optimization and validation of conventional and micellar LC methods for the analysis of methyltestosterone in sugar-coated pills.

Two isocratic liquid chromatographic methods (conventional and micellar) for the determination of methyltestosterone in sugar-coated pills using fluoxymesterone as internal standard have been developed and validated. In conventional liquid chromatography a mobile phase 45% water:acetonitrile 55% (v:v), a flow-rate 1 mlmin(-1) and a C(18) Hypersil ODS (250 x 4.6 mm, 5 microm) column (25 degrees C) were used. In micellar liquid chromatography the conditions were: mobile phase 40 mM sodium dodecyl sulfate: 10% propanol, flow-rate 0.5 mlmin(-1) and C(18) Hypersil ODS (150 x 3.0 mm, 5 microm) column (60 degrees C). For both methods, UV absorbance detection at 245 nm was used and a separation up to base line was achieved. Prior to HPLC analysis a simple sample preparation was required.

Anabolic Agents↗
PubMed1975

[Abnormal hypothalamic-hypophyseal regulation as a new endocrine sign in the testicular feminisation syndrome (author's transl)].

In a 38-year-old woman with the testicular feminisation syndrome (TFS) there were increased serum levels of LH and FSH, despite normal testosterone levels, ranging from 808 to 1330 ng/dl. The patient exhibited complete end-organ resistance to androgens, as well as decreased free testosterone fraction of 1.5 percent. On stimulation with LH-RH there was enhanced LH reaction to 15 ng/ml, while FSH levels remained unchanged. Fluoxymesterone did not suppress LH and testosterone, as it did in normal controls. But the functional Leydig-cell reserve could be normally stimulated with HCG. Our results apparently confirm the suspected reduction in sensitivity of the hypothalamic-pituitary axis to androgens and suggest that this plays an important part in the pathogenesis of TES.

Adult↗
PubMed1993

Effect of prepubertal gonadectomy and sex steroid treatment on the growth and lymphocyte populations of the rat thymus.

The age at which rats are most sensitive to prepubertal gonadectomy, in terms of thymic growth, was investigated. Gonadectomy enhanced thymic growth at each age; the greatest difference in thymic weight between gonadectomized and intact animals occurred in male rats gonadectomized at 5 weeks of age (64%) and in female rats gonadectomized at 4-5 weeks of age (43-46%). The effect of various synthetic sex steroids on growth and lymphocyte populations of the thymus in gonadectomized rats was examined. Diethylstilboestrol, 1 mg per animal, inhibited thymic growth by more than 35% in both males and females. Ethinyloestradiol, 40 micrograms per animal, inhibited thymic growth by 26% in males but by only 4% in females. Fluoxymesterone, 10 mg per animal, inhibited thymic growth by more than 46% in both sexes. Norgestrel, 12 micrograms per animal, had no effect on thymic growth. The synthetic steroids that significantly inhibited thymic growth decreased the intensity and altered the localization of staining for total T cells (antibody clone MRC OX 19), T helper cells and macrophages (W 3/5), T cytotoxic/suppressor cells (MRC OX 8) and B cells (MRC OX 12).

Aging↗
PubMed1985

Cytotoxic chemotherapy and androgen priming in patients with advanced carcinoma of the prostate. A phase II trial of the Piedmont Oncology Association.

Twenty-three patients with advanced prostatic cancer refractory to hormonal therapy were entered into a phase II study of cytotoxic chemotherapy combined with androgen priming. Patients received vincristine 0.5 mg on day 1; fluoxymesterone 10 mg p.o. TID, days 1-5; methotrexate 4 mg/m2 p.o., days 1-7; and cyclophosphamide 500 mg/m2 I.V., day 8. Patients entered had no prior chemotherapy, most were symptomatic but ambulatory (18/23), and almost all had bone metastases (22/23). There were two stable responses and 14 progressions in 16 patients evaluable for response. Hematologic and gastrointestinal toxicities were substantial. Androgen priming was an unsatisfactory method of improving response in this trial.

Aged↗